34105-39-0Relevant articles and documents
Asymmetric hydrogenation of the C-C double bond of 1- and 1,2-methylated maleimides with cultured suspension cells of Marchantia polymorpha
Hegazy, Mohamed-Elamir F.,Shishido, Kozo,Hirata, Toshifumi
, p. 1859 - 1862 (2006)
Suspension cultured cells of Marchantia polymorpha have the potential to hydrogenate the C-C double bonds of 2-methyl- and 2,3-dimethylmaleimide derivatives to give enantiomerically pure (2R)-2-methyl- and (2R,3R)-2,3-dimethylsuccinimide derivatives, resp
N-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting Pseudomonas aeruginosa Elastase and Clostridium Collagenases
Konstantinovi?, Jelena,Yahiaoui, Samir,Alhayek, Alaa,Haupenthal, J?rg,Sch?nauer, Esther,Andreas, Anastasia,Kany, Andreas M.,Müller, Rolf,Koehnke, Jesko,Berger, Fabian K.,Bischoff, Markus,Hartmann, Rolf W.,Brandstetter, Hans,Hirsch, Anna K. H.
, p. 8359 - 8368 (2020/09/16)
In light of the global antimicrobial-resistance crisis, there is an urgent need for novel bacterial targets and antibiotics with novel modes of action. It has been shown that Pseudomonas aeruginosa elastase (LasB) and Clostridium histolyticum (Hathewaya histolytica) collagenase (ColH) play a significant role in the infection process and thereby represent promising antivirulence targets. Here, we report novel N-Aryl-3-mercaptosuccinimide inhibitors that target both LasB and ColH, displaying potent activities in vitro and high selectivity for the bacterial over human metalloproteases. Additionally, the inhibitors demonstrate no signs of cytotoxicity against selected human cell lines and in a zebrafish embryo toxicity model. Furthermore, the most active ColH inhibitor shows a significant reduction of collagen degradation in an ex vivo pig-skin model.
A highly efficient and stereoselective cycloaddition of nitrones to N-arylitaconimides
Teterina, Polina S.,Efremova, Mariia M.,Sirotkina, Ekaterina V.,Novikov, Alexander S.,Khoroshilova, Olesya V.,Molchanov, Alexander P.
supporting information, (2019/08/26)
The 1,3-dipolar cycloaddition of keto- and aldonitrones with N-arylitaconimides proceeds regioselectively giving only 5-spiroisoxazolidines. In the case of aldonitrones the reaction proceeds with high diastereoselectivity. A range of the obtained adducts
